STTR Phase I: ACC Synthesis - a Way to Create Safer, Efficacious and Inexpensive Single Enantiomers

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This award is funded under the American Recovery and Reinvestment Act of 2009 (Public Law 111-5).This Small Business Technology Transfer (STTR) Phase I project propose a new method of producing enantiomerically pure ketones through the use of ACC chiral auxiliaries. The synthesis of single enantiomer drugs is an extremely important aspect of drug development. Current methods to both produce and/or isolate single enantiomer compounds are quite limited, and those existing methods can be expensive and difficult to carry out, thus preventing their application on large scale manufacturing. ACCs can be readily synthesized from commercially available starting materials in an efficient and cost effective way. They are easily introduced into the parent ketone, and can be easily recycled upon removal. Moreover, their inherent reactivity overcomes the practical limitations of current methods, making them amenable to industrial applications.The broader impacts of this research are: Development and subsequent FDA approval for new therapeutic agents has become increasingly difficult. R&D costs for a new drug are now in excess of $800 million and FDA has introduced more strict regulations and extensive clinical trials. Additionally, there have been several cases of leading companies suffering significant financial losses because of class action lawsuits from their drugs causing unforeseen sideeffects after reaching the market. The pharmaceutical industry is currently struggling to find solutions to overcome the new challenges in the field of drug development and the public has seen limited advances. Our innovative synthetic method will facilitate the production of single enantiomer drug formulations, which can contribute directly to finding solutions to the growing crisis facing the pharmaceutical industry.